A structure-activity relationship study of potent TIQ15-derived CXCR4 antagonists is reported. In this investigation, the TIQ15 side-chain was constrained to improve its drug properties. The cyclohexylamino congener was found to be a potent CXCR4 inhibitor (IC = 33 nM in CXCL12-mediated Ca flux) with enhanced stability in liver microsomes and reduced inhibition of CYP450 (2D6). The improved CXCR4 antagonist has potential therapeutic application as a single agent or combinatory anticancer therapy.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5807867 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.7b00406 | DOI Listing |
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